EA201291327A1 - Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5 - Google Patents
Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5Info
- Publication number
- EA201291327A1 EA201291327A1 EA201291327A EA201291327A EA201291327A1 EA 201291327 A1 EA201291327 A1 EA 201291327A1 EA 201291327 A EA201291327 A EA 201291327A EA 201291327 A EA201291327 A EA 201291327A EA 201291327 A1 EA201291327 A1 EA 201291327A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- mglur5
- substituted
- compounds
- positive allosteric
- allosteric modulators
- Prior art date
Links
- 230000003281 allosteric effect Effects 0.000 title abstract 2
- 101150087728 Grm5 gene Proteins 0.000 title 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 abstract 2
- 229930195712 glutamate Natural products 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- IJXDURUAYOKSIS-UHFFFAOYSA-N 6-methylpyridine-3-carboxamide Chemical class CC1=CC=C(C(N)=O)C=N1 IJXDURUAYOKSIS-UHFFFAOYSA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Emergency Medicine (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34779510P | 2010-05-24 | 2010-05-24 | |
| PCT/US2011/037775 WO2011149963A1 (en) | 2010-05-24 | 2011-05-24 | Substituted-6-methylnicotinamides as mglur5 positive allosteric modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201291327A1 true EA201291327A1 (ru) | 2013-05-30 |
Family
ID=45004338
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201291327A EA201291327A1 (ru) | 2010-05-24 | 2011-05-24 | Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5 |
Country Status (10)
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8969389B2 (en) | 2010-05-24 | 2015-03-03 | Vanderbilt University | Substituted 6-methylnicotinamides as mGluR5 positive allosteric modulators |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130252943A1 (en) * | 2012-02-29 | 2013-09-26 | Vanderbilt University | Bicyclic oxazole lactams as allosteric modulators of mglur5 receptors |
| CN106146391A (zh) | 2015-04-15 | 2016-11-23 | 中国科学院上海药物研究所 | 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 |
| US9987242B2 (en) | 2015-05-05 | 2018-06-05 | Northwestern University | Treatment of Levodopa-induced Dyskinesias |
| CA3012832A1 (en) | 2016-02-05 | 2017-08-10 | Denali Therapeutics Inc. | N-azepinyl-carboxamide inhibitors of receptor-interacting protein kinase1 |
| RS63203B1 (sr) | 2016-12-09 | 2022-06-30 | Denali Therapeutics Inc | Jedinjenja korisna kao inhibitori ripk1 |
| CN114437025B (zh) * | 2020-11-05 | 2023-08-25 | 上海零诺生物科技有限公司 | 消旋6-甲基烟碱及其制备方法、以及应用 |
| EP4463229A1 (en) | 2022-01-12 | 2024-11-20 | Denali Therapeutics Inc. | Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5438033A (en) * | 1991-06-12 | 1995-08-01 | E. I. Dupont De Nemours And Company | Substituted pyridine herbicides |
| EP0533130A1 (de) * | 1991-09-19 | 1993-03-24 | Hoechst Aktiengesellschaft | 2-Hydroxymethylpyridine, die entsprechenden Pyridin-N-oxide und ihre Derivate, Verfahren zu ihrer Herstellung sowie deren Verwendung |
| GB9417532D0 (en) * | 1994-08-31 | 1994-10-19 | Zeneca Ltd | Aromatic compounds |
| US6608058B2 (en) | 2000-04-17 | 2003-08-19 | Dong Wha Pharm. Ind. Co., Ltd. | 6-methylnicotinamide derivatives as antiviral agents |
| JP4795022B2 (ja) | 2003-09-30 | 2011-10-19 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘテロ環化合物を含有する新規な抗真菌剤 |
| CA2555402A1 (en) * | 2004-02-12 | 2005-09-01 | Celine Bonnefous | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
| CN101321731A (zh) * | 2005-12-20 | 2008-12-10 | 诺瓦提斯公司 | 作为代谢型谷氨酸受体调节剂的烟酸衍生物 |
| AR058554A1 (es) * | 2005-12-20 | 2008-02-13 | Novartis Ag | Compuestos heterociclicos nitrogenados de 6 miembros sustituidos, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por mglur5. |
| AU2007343139A1 (en) * | 2006-12-21 | 2008-07-17 | Pfizer Products Inc. | Compounds having both angiotensin II receptor antagonism and PPARy activating activities |
| CN101600715A (zh) * | 2006-12-21 | 2009-12-09 | 辉瑞产品公司 | 具有血管紧张素II受体拮抗作用和PPARγ活化活性的化合物 |
| JP5622568B2 (ja) * | 2007-06-03 | 2014-11-12 | バンダービルト ユニバーシティ | ベンズアミドｍＧｌｕＲ５の正のアロステリック調節因子ならびにその作製および使用方法 |
| US8034806B2 (en) * | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| MX2012003394A (es) * | 2009-09-21 | 2012-08-15 | Univ Vanderbilt | Analogos de la nicotinamida de o-bencilo como moduladores alostéricos positivos del mglur5. |
| US20120251427A1 (en) | 2009-11-25 | 2012-10-04 | Josef Filtvedt | Reactor and method for production of silicon |
| EP2575461A4 (en) | 2010-05-24 | 2013-12-18 | Univ Vanderbilt | SUBSTITUTED 6-METHYLNICOTINAMIDES USEFUL AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR5 |
-
2011
- 2011-05-24 EP EP11787265.5A patent/EP2575461A4/en not_active Withdrawn
- 2011-05-24 CA CA2799966A patent/CA2799966A1/en not_active Abandoned
- 2011-05-24 JP JP2013512170A patent/JP2013526610A/ja active Pending
- 2011-05-24 US US13/114,958 patent/US8969389B2/en not_active Expired - Fee Related
- 2011-05-24 MX MX2012013560A patent/MX2012013560A/es not_active Application Discontinuation
- 2011-05-24 AU AU2011258389A patent/AU2011258389A1/en not_active Abandoned
- 2011-05-24 KR KR1020127033660A patent/KR20130122531A/ko not_active Withdrawn
- 2011-05-24 CN CN2011800335387A patent/CN103037693A/zh active Pending
- 2011-05-24 EA EA201291327A patent/EA201291327A1/ru unknown
- 2011-05-24 WO PCT/US2011/037775 patent/WO2011149963A1/en active Application Filing
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8969389B2 (en) | 2010-05-24 | 2015-03-03 | Vanderbilt University | Substituted 6-methylnicotinamides as mGluR5 positive allosteric modulators |
Also Published As
| Publication number | Publication date |
|---|---|
| US8969389B2 (en) | 2015-03-03 |
| KR20130122531A (ko) | 2013-11-07 |
| US20110294858A1 (en) | 2011-12-01 |
| AU2011258389A1 (en) | 2012-12-06 |
| EP2575461A1 (en) | 2013-04-10 |
| WO2011149963A1 (en) | 2011-12-01 |
| CA2799966A1 (en) | 2011-12-01 |
| EP2575461A4 (en) | 2013-12-18 |
| JP2013526610A (ja) | 2013-06-24 |
| CN103037693A (zh) | 2013-04-10 |
| MX2012013560A (es) | 2013-03-05 |
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